The Sound of Evolution
Mercaptopurine
Mechanism of action:
Mercaptopurine is a thiopurine derivative. Mercaptopurine itself is a prodrug. After entering the cell, it is converted by hypoxanthine-guanine phosphoribosyltransferase (HGPRT) into thioinosine monophosphate, which is then further converted into several active thiopurine nucleotides. These active metabolites inhibit enzymes involved in purine synthesis, leading to reduced production of IMP, AMP, and GMP. As a result, the cell cannot obtain sufficient purine precursors for DNA and RNA synthesis.
Reference(s):
1. Dubinsky MC et al. (2004). Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety. Clin Gastroenterol Hepatol.
2. Zhou Y et al. (2024). TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res.